TY - JOUR
T1 - Transdermal delivery of tetrahydrocannabinol
AU - Touitou, Elka
AU - Fabin, Boris
AU - Dany, Sanda
AU - Almog, Shlomo
PY - 1988/4
Y1 - 1988/4
N2 - The skin permeation behavior of a tetrahydrocannabinol (THC) is described for the first time. In the design of transdermal delivery systems, Δ8-THC was chosen over Δ9-THC due to the former's better stability and its lower psychotropic potency. Sk permeation kinetic parameters were established through rat and human skin in vitro. The rat skin was found to be about 13-fold more permeable to Δ8-THC than the human skin. Autoradiographs showed that 24 h after application the drug was concentrated in the stratum corneum, in the upper epidermis, and around the hair follicles, indicating that THC penetrates the skin through the lipophilic pathways. A transdermal formulation containing oleic acid as a permeation enhancer was tested in rats. A serum level of about 50 ng/ml cross-reacting cannabinoids (THC + metabolites) was maintained for about 24 h, indicating a sustained delivery of THC to the bloodstream. The transdermal preparation presented in this study is designed for future clinical studies.
AB - The skin permeation behavior of a tetrahydrocannabinol (THC) is described for the first time. In the design of transdermal delivery systems, Δ8-THC was chosen over Δ9-THC due to the former's better stability and its lower psychotropic potency. Sk permeation kinetic parameters were established through rat and human skin in vitro. The rat skin was found to be about 13-fold more permeable to Δ8-THC than the human skin. Autoradiographs showed that 24 h after application the drug was concentrated in the stratum corneum, in the upper epidermis, and around the hair follicles, indicating that THC penetrates the skin through the lipophilic pathways. A transdermal formulation containing oleic acid as a permeation enhancer was tested in rats. A serum level of about 50 ng/ml cross-reacting cannabinoids (THC + metabolites) was maintained for about 24 h, indicating a sustained delivery of THC to the bloodstream. The transdermal preparation presented in this study is designed for future clinical studies.
KW - Antiemetic
KW - Skin autoradiograph
KW - Skin permeation
KW - Tetrahydrocannabinol
KW - Transdermal delivery
UR - http://www.scopus.com/inward/record.url?scp=0023923402&partnerID=8YFLogxK
U2 - 10.1016/0378-5173(88)90052-X
DO - 10.1016/0378-5173(88)90052-X
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AN - SCOPUS:0023923402
SN - 0378-5173
VL - 43
SP - 9
EP - 15
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -